JP4608215B2 - キナゾリン化合物 - Google Patents

キナゾリン化合物 Download PDF

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Publication number
JP4608215B2
JP4608215B2 JP2003564036A JP2003564036A JP4608215B2 JP 4608215 B2 JP4608215 B2 JP 4608215B2 JP 2003564036 A JP2003564036 A JP 2003564036A JP 2003564036 A JP2003564036 A JP 2003564036A JP 4608215 B2 JP4608215 B2 JP 4608215B2
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Prior art keywords
alkyl
fluoro
methoxyquinazoline
defined above
methyl
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Expired - Fee Related
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Japanese (ja)
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JP2005522428A (ja
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ヘンネキン,ローレント・フランコイス・アンドレ
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アストラゼネカ アクチボラグ
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Reproductive Health (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
JP2003564036A 2002-02-01 2003-01-28 キナゾリン化合物 Expired - Fee Related JP4608215B2 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02290242 2002-02-01
PCT/GB2003/000343 WO2003064413A1 (fr) 2002-02-01 2003-01-28 Composes de quinazoline

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2009297126A Division JP2010100642A (ja) 2002-02-01 2009-12-28 キナゾリン化合物

Publications (2)

Publication Number Publication Date
JP2005522428A JP2005522428A (ja) 2005-07-28
JP4608215B2 true JP4608215B2 (ja) 2011-01-12

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JP2003564036A Expired - Fee Related JP4608215B2 (ja) 2002-02-01 2003-01-28 キナゾリン化合物
JP2009297126A Pending JP2010100642A (ja) 2002-02-01 2009-12-28 キナゾリン化合物

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2009297126A Pending JP2010100642A (ja) 2002-02-01 2009-12-28 キナゾリン化合物

Country Status (29)

Country Link
US (3) US7268230B2 (fr)
EP (2) EP1474420B1 (fr)
JP (2) JP4608215B2 (fr)
KR (1) KR101093345B1 (fr)
CN (2) CN101607958A (fr)
AR (1) AR038476A1 (fr)
AT (1) ATE549329T1 (fr)
AU (1) AU2003202094B2 (fr)
BR (1) BR0307151A (fr)
CA (1) CA2473572C (fr)
CY (1) CY1112835T1 (fr)
DK (1) DK1474420T3 (fr)
ES (1) ES2381781T3 (fr)
HK (1) HK1070367A1 (fr)
HU (1) HUP0402588A3 (fr)
IL (2) IL163022A (fr)
IS (1) IS7362A (fr)
MX (1) MXPA04007459A (fr)
MY (1) MY144042A (fr)
NO (1) NO328731B1 (fr)
NZ (1) NZ534171A (fr)
PL (1) PL371486A1 (fr)
PT (1) PT1474420E (fr)
RU (3) RU2362775C1 (fr)
SI (1) SI1474420T1 (fr)
TW (1) TWI337866B (fr)
UA (1) UA81619C2 (fr)
WO (1) WO2003064413A1 (fr)
ZA (1) ZA200405908B (fr)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS49779B (sr) * 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
ATE482946T1 (de) * 1999-02-10 2010-10-15 Astrazeneca Ab Chinazolinderivate als angiogenesehemmer und zwischenprodukte dafür
MXPA02004366A (es) 1999-11-05 2002-11-07 Astrazeneca Ab Derivados de quinazolina como inhibidores vegf.
ES2267748T3 (es) * 2000-04-07 2007-03-16 Astrazeneca Ab Compuestos de quinazolina.
HN2002000067A (es) * 2001-03-23 2003-10-24 Bayer Healthcare Llc Inhibidores de la rho - quinasa.
EP1474420B1 (fr) 2002-02-01 2012-03-14 AstraZeneca AB Composes de quinazoline
EP1521747B1 (fr) 2002-07-15 2018-09-05 Symphony Evolution, Inc. Modulateurs de kinase de type recepteur et procedes d'utilisation
SI1562955T1 (sl) 2002-11-04 2008-06-30 Astrazeneca Ab Derivati kinazolina kot inhibitorji Src-triozin kinaze
GB0316127D0 (en) * 2003-07-10 2003-08-13 Astrazeneca Ab Combination therapy
GB0318422D0 (en) * 2003-08-06 2003-09-10 Astrazeneca Ab Chemical compounds
DE10340485B4 (de) 2003-09-03 2015-05-13 Morphochem AG Aktiengesellschaft für kombinatorische Chemie Verfahren zur Herstellung von Oxazolidinon-Chinolon Hybriden
DE602004004811T2 (de) * 2003-09-19 2007-11-22 Astrazeneca Ab Chinazolinderivate
CA2537812C (fr) 2003-09-26 2013-01-22 Exelixis, Inc. Modulateurs de c-met et procede d'utilisation
GB0330002D0 (en) 2003-12-24 2004-01-28 Astrazeneca Ab Quinazoline derivatives
GEP20084439B (en) 2004-01-23 2008-07-25 Amgen Inc Nitrogen-containing heterocyclic derivatives and pharmaceutical use thereof
EP1711495A2 (fr) 2004-01-23 2006-10-18 Amgen Inc. Quinolines, chinazolines, pyridines et pyrimidines et leur utilsation dans le traitement d'inflammation, angiogenèse et le cancer
MX2007004403A (es) 2004-10-12 2007-04-27 Astrazeneca Ab Derivados de quinazolina.
CA2587642C (fr) 2004-11-30 2013-04-09 Amgen Inc. Heterocycles substitues et methodes d'utilisation
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
US7825244B2 (en) 2005-06-10 2010-11-02 Janssen Pharmaceutica Nv Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis
US8071768B2 (en) 2005-06-10 2011-12-06 Janssen Pharmaceutica, N.V. Alkylquinoline and alkylquinazoline kinase modulators
AR054608A1 (es) 2005-08-08 2007-06-27 Actelion Pharmaceuticals Ltd Derivados de oxazolidinona enlazados a quinolonas como antibacterianos
GB0519879D0 (en) 2005-09-30 2005-11-09 Astrazeneca Ab Chemical process
GB0523810D0 (en) * 2005-11-23 2006-01-04 Astrazeneca Ab Pharmaceutical compositions
KR101415354B1 (ko) 2006-02-22 2014-07-04 4에스체 악티엔게젤샤프트 Eg5 키네신 조절제로서의 인돌로피리딘
JP2009528336A (ja) * 2006-03-02 2009-08-06 アストラゼネカ アクチボラグ キノリン誘導体
UY30183A1 (es) * 2006-03-02 2007-10-31 Astrazeneca Ab Derivados de quinolina
US7851623B2 (en) * 2006-11-02 2010-12-14 Astrazeneca Ab Chemical process
WO2008063888A2 (fr) 2006-11-22 2008-05-29 Plexxikon, Inc. Composés modulant l'activité de c-fms et/ou de c-kit et utilisations associées
WO2008079909A1 (fr) * 2006-12-21 2008-07-03 Plexxikon, Inc. Composés et méthodes de modulation des kinases, et indications connexes
US7648979B2 (en) 2007-02-07 2010-01-19 Hoffmann-La Roche Inc. 5-amido-(1H-indol-2-yl)-piperazin-1-yl-methanone derivatives
US7507736B2 (en) 2007-02-07 2009-03-24 Hoffmann-La Roche Inc. Indol-2-yl-piperazin-1-yl-methanone derivatives
US20080190689A1 (en) * 2007-02-12 2008-08-14 Ballard Ebbin C Inserts for engine exhaust systems
BRPI0814423B1 (pt) 2007-07-17 2022-04-19 Plexxikon, Inc Compostos que modulam quinase e composição farmacêutica compreendendo os mesmos
US7795254B2 (en) * 2007-10-29 2010-09-14 Amgen Inc. Benzomorpholine derivatives and methods of use
ES2444128T3 (es) 2008-05-13 2014-02-24 Astrazeneca Ab Nueva SAL-554
CA2995880C (fr) 2009-01-16 2021-01-05 Exelixis, Inc. Procedes de preparation de n-(4-{[6,7-bis(methyloxy)quinolein-4-yl]oxy}phenyl)(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
WO2010092371A1 (fr) 2009-02-10 2010-08-19 Astrazeneca Ab Dérivés de triazolo[4,3-b]pyridazine et leurs utilisations contre le cancer de la prostate
AR078033A1 (es) 2009-04-03 2011-10-12 Plexxikon Inc Una dispersion solida, que contiene al compuesto {3-[5-(4-(cloro-fenil)-1h-pirrolo[2,3-b]piridina-3-carbonil]-2,4-difluor-fenil}-amida del acido propano-1-sulfonico, composiciones y formulaciones que comprenden a dicha dispersion solida; metodos para fabricar dicha dispersion solida, formas 1 y 2 de
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
ES2633317T3 (es) 2009-11-06 2017-09-20 Plexxikon, Inc. Compuestos y métodos para la modulación de quinasas, e indicaciones para ello
MA34948B1 (fr) 2011-02-07 2014-03-01 Plexxikon Inc Composes et procedes de modulation de kinase, et leurs indications
TWI558702B (zh) 2011-02-21 2016-11-21 普雷辛肯公司 醫藥活性物質的固態形式
AR086411A1 (es) * 2011-05-20 2013-12-11 Nippon Soda Co Compuesto heterociclico conteniendo nitrogeno y fungicida para el uso en agricultura y jardineria
TWI557109B (zh) * 2011-12-29 2016-11-11 財團法人生物技術開發中心 喹唑啉化合物作為激酶抑制劑及其應用
CN103288756B (zh) * 2012-02-29 2016-04-20 江苏先声药物研究有限公司 一种喹唑啉中间体的甲醇溶剂合物及其制备方法
US9242355B2 (en) 2012-04-17 2016-01-26 Black & Decker Inc. Illuminated power tool
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
AU2014216178B2 (en) 2013-02-15 2018-06-28 KALA BIO, Inc. Therapeutic compounds and uses thereof
WO2015066584A1 (fr) * 2013-11-01 2015-05-07 Kala Pharmaceuticals, Inc. Formes cristallines de composés thérapeutiques et utilisations de celles-ci
ES2831625T3 (es) 2013-02-20 2021-06-09 Kala Pharmaceuticals Inc Compuestos terapéuticos y sus usos
US9688688B2 (en) * 2013-02-20 2017-06-27 Kala Pharmaceuticals, Inc. Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof
US9890173B2 (en) 2013-11-01 2018-02-13 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
JP6426194B2 (ja) * 2013-11-01 2018-11-21 カラ ファーマシューティカルズ インコーポレイテッド 治療用化合物の結晶形態及びその使用
CN108473435A (zh) 2015-10-05 2018-08-31 纽约市哥伦比亚大学理事会 自噬潮和磷脂酶d的活化剂以及包括tau的蛋白聚集体的清除和蛋白质病的治疗
CN105461718A (zh) * 2016-01-13 2016-04-06 苏州莱安医药化学技术有限公司 一种5-溴-7-氮杂吲哚的合成工艺
RU2742771C2 (ru) * 2016-08-31 2021-02-10 Цзянсу Хэнжуй Медицин Ко., Лтд. Производное оксопиколинамида, способ его получения и его фармацевтическое применение
EP3509422A4 (fr) 2016-09-08 2020-05-20 Kala Pharmaceuticals, Inc. Formes cristallines de composés thérapeutiques et leurs utilisations
US10392399B2 (en) 2016-09-08 2019-08-27 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
BR112019004463A2 (pt) 2016-09-08 2019-05-28 Kala Pharmaceuticals Inc formas cristalinas de compostos terapêuticos, seus processos de obtenção e seus métodos de uso
CN107840843A (zh) * 2017-10-17 2018-03-27 浙江工业大学义乌科学技术研究院有限公司 一种西地尼布中间体的合成方法
CA3079673A1 (fr) * 2017-10-20 2019-04-25 Kala Pharmaceuticals, Inc. Inhibiteurs de ret9 et vegfr2
CN112996784B (zh) * 2018-09-18 2023-05-30 北京越之康泰生物医药科技有限公司 吲哚衍生物及其在医药上的应用

Family Cites Families (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU174215B (hu) 1976-12-15 1979-11-28 Richter Gedeon Vegyeszet Sposob poluchenija novykh proizvodnykh piperazina i kislotnykh additivnykh i chetvjortichnykh solej
IL81307A0 (en) 1986-01-23 1987-08-31 Union Carbide Agricult Method for reducing moisture loss from plants and increasing crop yield utilizing nitrogen containing heterocyclic compounds and some novel polysubstituted pyridine derivatives
IL89029A (en) 1988-01-29 1993-01-31 Lilly Co Eli Fungicidal quinoline and cinnoline derivatives, compositions containing them, and fungicidal methods of using them
US5411963A (en) * 1988-01-29 1995-05-02 Dowelanco Quinazoline derivatives
DE4022414A1 (de) * 1990-07-13 1992-01-16 Bayer Ag Substituierte pyrrolo-pyridine
US5710158A (en) * 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5480883A (en) * 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US6645969B1 (en) * 1991-05-10 2003-11-11 Aventis Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
US5714493A (en) * 1991-05-10 1998-02-03 Rhone-Poulenc Rorer Pharmaceuticals, Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
SG64322A1 (en) * 1991-05-10 1999-04-27 Rhone Poulenc Rorer Int Bis mono and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
US5721237A (en) * 1991-05-10 1998-02-24 Rhone-Poulenc Rorer Pharmaceuticals Inc. Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
FR2687402B1 (fr) * 1992-02-14 1995-06-30 Lipha Nouveaux azaindoles, procedes de preparation et medicaments les contenant.
US5212195A (en) * 1992-05-13 1993-05-18 Syntex (U.S.A.) Inc. Substituted indole antagonists derivatives which are angiotensin II
GB9323290D0 (en) 1992-12-10 1994-01-05 Zeneca Ltd Quinazoline derivatives
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
CA2183655C (fr) * 1994-02-23 2001-03-06 Lee D. Arnold Derives de la quinazoline a substitution 4-heterocyclyle, procedes d'elaboration et utilisations correspondantes comme agents anticancereux
WO1995024190A2 (fr) 1994-03-07 1995-09-14 Sugen, Inc. Inhibiteurs de tyrosine-kinase receptrice destines a inhiber les troubles lies a la proliferation cellulaire et compositions les contenant
GB9505651D0 (en) 1995-03-21 1995-05-10 Agrevo Uk Ltd AgrEvo UK Limited
FR2732969B1 (fr) * 1995-04-14 1997-05-16 Adir Nouveaux composes pyridiniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US6046206A (en) * 1995-06-07 2000-04-04 Cell Pathways, Inc. Method of treating a patient having a precancerous lesions with amide quinazoline derivatives
GB9514265D0 (en) 1995-07-13 1995-09-13 Wellcome Found Hetrocyclic compounds
WO1997017329A1 (fr) 1995-11-07 1997-05-15 Kirin Beer Kabushiki Kaisha Derives de quinoline et derives de quinazoline inhibant l'autophosphorylation d'un recepteur de facteur de croissance originaire de plaquettes, et compositions pharmaceutiques les contenant
GB9624482D0 (en) * 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
EP0880508B1 (fr) * 1996-02-13 2003-04-16 AstraZeneca AB Derives de la quinazoline utilises comme inhibiteurs du vegf
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
ATE211134T1 (de) * 1996-03-05 2002-01-15 4-anilinochinazolin derivate
EP0888310B1 (fr) * 1996-03-15 2005-09-07 AstraZeneca AB Derives de cinnoline et leur emploi comme medicaments
DE19614718A1 (de) 1996-04-15 1997-10-16 Hoechst Schering Agrevo Gmbh Substituierte Pyridine/Pyrimidine, Verfahren zu ihrer Herstellung, und ihre Verwendung als Schädlingsbekämpfungsmittel
GB9707800D0 (en) * 1996-05-06 1997-06-04 Zeneca Ltd Chemical compounds
CA2258548C (fr) 1996-06-24 2005-07-26 Pfizer Inc. Derives tricycliques substitues par phenylamino, destines au traitement des maladies hyperproliferatives
AR007857A1 (es) 1996-07-13 1999-11-24 Glaxo Group Ltd Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen.
IL128994A (en) 1996-09-25 2004-12-15 Zeneca Ltd History of quinoline and naphthyridine and their salts, processes for their preparation, pharmaceutical preparations containing them and their use as medicines
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
EP0837063A1 (fr) 1996-10-17 1998-04-22 Pfizer Inc. Dérivés de 4-aminoquinazoline
US6225318B1 (en) * 1996-10-17 2001-05-01 Pfizer Inc 4-aminoquinazolone derivatives
CA2291709A1 (fr) 1997-05-30 1998-12-03 Merck & Co., Inc. Nouveaux inhibiteurs d'angiogenese
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
ZA986729B (en) * 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
DE69838172T2 (de) 1997-08-22 2008-04-10 Astrazeneca Ab Oxindolylchinazolinderivate als angiogenesehemmer
US6162804A (en) * 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
GB9721437D0 (en) 1997-10-10 1997-12-10 Glaxo Group Ltd Heteroaromatic compounds and their use in medicine
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
GB9800575D0 (en) * 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
US6172071B1 (en) 1998-07-30 2001-01-09 Hughes Institute Lipid-lowering quinazoline derivative
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
KR100860295B1 (ko) 1998-10-08 2008-09-25 아스트라제네카 아베 퀴나졸린 유도체
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB2345486A (en) 1999-01-11 2000-07-12 Glaxo Group Ltd Heteroaromatic protein tyrosine kinase inhibitors
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
ES2281591T3 (es) 1999-01-22 2007-10-01 Kirin Beer Kabushiki Kaisha Derivados de n-((quinolinil)oxil)-fenil)-urea y de n-((quinazolinil)oxil)-fenil)-urea con actividad antitumoral.
JP3270834B2 (ja) 1999-01-27 2002-04-02 ファイザー・プロダクツ・インク 抗がん剤として有用なヘテロ芳香族二環式誘導体
UA71945C2 (en) 1999-01-27 2005-01-17 Pfizer Prod Inc Substituted bicyclic derivatives being used as anticancer agents
ATE482946T1 (de) 1999-02-10 2010-10-15 Astrazeneca Ab Chinazolinderivate als angiogenesehemmer und zwischenprodukte dafür
DE19911509A1 (de) 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
TWI262914B (en) * 1999-07-02 2006-10-01 Agouron Pharma Compounds and pharmaceutical compositions for inhibiting protein kinases
KR20020029419A (ko) 1999-07-07 2002-04-18 다비드 에 질레스 퀴나졸린 유도체
EE05107B1 (et) 1999-10-19 2008-12-15 Merck & Co., Inc. Türosiinkinaasi pärssiv ühend, seda sisaldav farmatseutiline kompositsioon ning ühendi kasutamine
MXPA02004366A (es) 1999-11-05 2002-11-07 Astrazeneca Ab Derivados de quinazolina como inhibidores vegf.
AU2001235804A1 (en) * 2000-03-06 2001-09-17 Astrazeneca Ab Therapy
GB0008269D0 (en) 2000-04-05 2000-05-24 Astrazeneca Ab Combination chemotherapy
ES2267748T3 (es) * 2000-04-07 2007-03-16 Astrazeneca Ab Compuestos de quinazolina.
KR20030013433A (ko) 2000-05-31 2003-02-14 아스트라제네카 아베 혈관 손상 활성을 가진 인돌 유도체
UA73993C2 (uk) * 2000-06-06 2005-10-17 Астразенека Аб Хіназолінові похідні для лікування пухлин та фармацевтична композиція
AU6623301A (en) 2000-07-07 2002-01-21 Angiogene Pharm Ltd Colchinol derivatives as vascular damaging agents
EE200300015A (et) 2000-07-07 2004-10-15 Angiogene Pharmaceuticals Limited Kolhinooli derivaadid kui angiogeneesi inhibiitorid
WO2002012226A1 (fr) * 2000-08-09 2002-02-14 Astrazeneca Ab Derives de la quinoline presentant une activite inhibant le facteur de croissance vegf
ES2317923T3 (es) 2000-08-09 2009-05-01 Astrazeneca Ab Compuestos de cinolina.
EP1311500A2 (fr) 2000-08-09 2003-05-21 AstraZeneca AB Derives d'indole, d'azaindole et indazole ayant une activite inhibitrice de vegf
BR0113358A (pt) * 2000-08-21 2003-07-01 Astrazeneca Ab Derivado de quinazolina ou de um seu sal farmaceuticamente aceitável, processo para a sua preparação, composição farmacêutica, e, uso do derivado ou de um seu sal farmaceuticamente aceitável
AU2002323406A1 (en) 2001-08-30 2003-03-18 Merck And Co., Inc. Tyrosine kinase inhibitors
US7169788B2 (en) 2001-10-30 2007-01-30 Merck & Co., Inc. Tyrosine kinase inhibitors
GB0126433D0 (en) * 2001-11-03 2002-01-02 Astrazeneca Ab Compounds
ES2320980T3 (es) * 2001-11-03 2009-06-01 Astrazeneca Ab Derivados de quinazolina como agentes antitumorales.
GB0126879D0 (en) * 2001-11-08 2002-01-02 Astrazeneca Ab Combination therapy
EP1474420B1 (fr) 2002-02-01 2012-03-14 AstraZeneca AB Composes de quinazoline
KR20050056190A (ko) * 2002-08-09 2005-06-14 아스트라제네카 아베 암의 치료에서의 방사선 요법과 함께 혈관 내피 성장 인자수용체의 억제제인 zd6474의 병행 치료
GB0305142D0 (en) * 2003-03-06 2003-04-09 Eisai London Res Lab Ltd Synthesis
GB0318423D0 (en) * 2003-08-06 2003-09-10 Astrazeneca Ab Chemical compounds
GB0318422D0 (en) * 2003-08-06 2003-09-10 Astrazeneca Ab Chemical compounds
GB0330002D0 (en) * 2003-12-24 2004-01-28 Astrazeneca Ab Quinazoline derivatives
US7117615B2 (en) * 2004-05-28 2006-10-10 Nike, Inc. Shoe with reversible upper
GB0519879D0 (en) * 2005-09-30 2005-11-09 Astrazeneca Ab Chemical process
US7851623B2 (en) * 2006-11-02 2010-12-14 Astrazeneca Ab Chemical process

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HUP0402588A2 (hu) 2005-05-30
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NO20043162L (no) 2004-07-22
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EP2292615A1 (fr) 2011-03-09
CA2473572C (fr) 2011-05-10
CA2473572A1 (fr) 2003-08-07
ZA200405908B (en) 2005-11-30
US7268230B2 (en) 2007-09-11
PL371486A1 (en) 2005-06-13
US8293902B2 (en) 2012-10-23
IL210785A0 (en) 2011-03-31
BR0307151A (pt) 2004-12-07
WO2003064413A1 (fr) 2003-08-07
IS7362A (is) 2004-07-22
ATE549329T1 (de) 2012-03-15
AU2003202094B2 (en) 2009-10-08
US20090156821A1 (en) 2009-06-18
US20050085465A1 (en) 2005-04-21
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NO328731B1 (no) 2010-05-03
DK1474420T3 (da) 2012-05-21
CY1112835T1 (el) 2016-02-10
UA81619C2 (ru) 2008-01-25
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IL163022A (en) 2012-10-31
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SI1474420T1 (sl) 2012-06-29
RU2365588C2 (ru) 2009-08-27
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US20080027069A1 (en) 2008-01-31
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